米尔塔扎是一种功能对抗剂,在心脏人类的H1H-胺受体
Thanh Hoai Pham1, Jonas M A Schlicht1, Britt Hofmann2
1Institute for Pharmacology and Toxicology, Medical Faculty, Martin-Luther-University Halle-Wittenberg, Magdeburger Straße 4, 06097, Halle (Saale), Germany.
发现抗抑郁药Mirtazapine可以阻断人类心脏的H1-胺受体. 这种对抗性可能会导致服用这种药物的患者心脏副作用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 心脏病学 心脏病学
- 神经科学是一个神经科学.
背景情况:
- 米尔塔扎平是一种非典型的抗抑郁药,已知与各种神经递质受体相互作用.
- 以前的研究表明,米尔塔扎因在体外和体内都与H1-胺受体结合.
- 密尔塔扎对心脏的影响,特别是对H1胺受体的影响,仍然在很大程度上未被探索.
研究的目的:
- 调查米尔塔萨平是否作为人类心脏H1-胺受体的对抗剂.
- 为了确定米尔塔扎与这些受体相互作用的潜在心脏影响.
主要方法:
- 使用过度表达人类H1-胺受体 (H1-TG) 和野生型 littermates (WT) 的转基因小鼠的隔离性心房制剂.
- 作为对H1-胺受体刺激的反应,测量了收缩力.
- 评估了mirtazapine对心脏手术患者中隔离的人类心房肌条 (HAP) 的影响.
主要成果:
- 米尔塔扎在小鼠前庭中表现出度和时间依赖的抑制H1-胺受体刺激的收缩.
- 最重要的是,米尔塔扎平在治疗度 (从100nM开始) 中显著降低了人类心房肌条中H1-基因组受体介导的收缩.
结论:
- 米尔塔扎平对抗人类心脏的H1-胺受体.
- 这种对抗性发生在临床相关度下.
- 米尔塔扎平可能会导致精神病患者的心脏不良反应.
更多相关视频
08:49Rapid In Situ Hybridization using Oligonucleotide Probes on Paraformaldehyde-prefixed Brain of Rats with Serotonin Syndrome
Published on: September 23, 2015
07:16Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
相关概念视频
Antidepressant Drugs: MAOIs and Other Agents
Antipsychotic Drugs: Typical and Atypical Agents
Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline...
Acid Suppressive Drugs for Peptic Ulcer Disease: Histamine H2-Receptor Antagonists
Sedatives and Hypnotics Drugs: Miscellaneous Agents
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
